- Synthesis and bioactivity of substituted benzoylguanidine derivatives as potent Na+/H+ exchanger inhibitors
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A novel series of substituted benzoylguanidine derivatives were designed and synthesized in order to evaluate their NHE1 inhibitory activity. Most of them were found to inhibit NHE1-mediated platelet swelling in a concentration-dependent manner, and eight compounds showed more potent NHE1 inhibitory activity than Cariporide. Compound 6f with an IC50 value of 1.08 × 10-10 molmiddot;L-1, was 39 times more potent than lead compound CPU-X-050420 in vitro tests. A novel series of 5-(2-(4-(2,3,4-trimethoxybenzyl)piperazin-1-yl)acetyl)benzoylguanidine derivatives 6a-6i have been synthesized and screened for their NHE1 inhibitory activity. Copyright
- Jin, Ning,Yang, Yun,Xu, Wenting,Yang, Xiaozhi,Gong, Guoqing,Xu, Yungen
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p. 333 - 340
(2012/05/19)
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- Bicyclyl or heterobicyclylmethanesulfonylamino-substituted n-hydroxyformamides
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Compounds of formula (I): R is hydrogen, alkyl, alkenyl, alkynyl, aryl, heteroaryl or heterocyclyl; and R1 is bicyclyl or heterobicyclyl, are useful in the treatment and prophylaxis of conditions mediated by s-CD23.
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- Pharmaceutically active bicyclic-heterocyclic amines
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The pharmaceutically active bicyclic heterocyclic amines (XXX) STR1 where W1 is --N= or --CH=; W3 is --N= or --CH=; W5 is --N= or --CR5 -- with the proviso that W5 is --CR5 -- when both W1 and W3 are --N= which are useful as pharmaceuticals in treating mild and/or moderate to severe head injury, subarachnoid hemorrhage and subsequent ischemic stroke, asthma and reduction of mucous formation/secretion in the lung and other diseases and injuries.
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- NOVEL ANTIHYPERTENSIVE AGENT
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This invention is to the compound 5-2-3-(1,3-benzodioxol-5-yl)-1-methylpropyl!amino!-1-hydroxyethyl!-2-methoxyben zamide having the formula, STR1 pharmaceutically acceptable salts and individual optical isomers thereof, pharmaceutical compositions comprising as the active ingredient the compound of Formula 1 or salts or isomers thereof and the use of said compound, or salt or isomer thereof or pharmaceutical composition comprising same in the treatment of hypertension.
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